Biologically Active Compounds Through Catalysis: Efficient Synthesis of N-(Heteroarylcarbonyl)-N′-(arylalkyl)piperazines.

ChemInform ◽  
2004 ◽  
Vol 35 (24) ◽  
Author(s):  
Kamal Kumar ◽  
Dirk Michalik ◽  
Ivette Garcia Castro ◽  
Annegret Tillack ◽  
Alexander Zapf ◽  
...  
Keyword(s):  
Biologically Active Compounds ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Active Compounds

scholarly journals Cover Picture: Biologically Active Compounds through Catalysis: Efficient Synthesis ofN-(Heteroarylcarbonyl)-N′-(arylalkyl)piperazines (Chem. Eur. J. 3/2004)

2004 ◽  
Vol 10 (3) ◽  
pp. 563-563
Author(s):  
Kamal Kumar ◽  
Dirk Michalik ◽  
Ivette Garcia Castro ◽  
Annegret Tillack ◽  
Alexander Zapf ◽  
...  
Keyword(s):  
Biologically Active Compounds ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Active Compounds

Biologically Active Compounds through Catalysis: Efficient Synthesis ofN-(Heteroarylcarbonyl)-N′-(arylalkyl)piperazines

2004 ◽  
Vol 10 (3) ◽  
pp. 746-757 ◽  
Author(s):  
Kamal Kumar ◽  
Dirk Michalik ◽  
Ivette Garcia Castro ◽  
Annegret Tillack ◽  
Alexander Zapf ◽  
...  
Keyword(s):  
Biologically Active Compounds ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Active Compounds

Microwave-accelerated and efficient synthesis of structurally diverse N-(2,2-diphenylvinyl)-β-oxoamides

2021 ◽  
Author(s):  
Xingpeng Chen ◽  
Yelong Lei ◽  
Duo Fu ◽  
Jiaxi Xu
Keyword(s):  
Ring Opening ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Active Compounds ◽  
Dicarbonyl Compounds ◽  
Synthetic Intermediates

N-(2,2-Diphenylvinyl)-β-oxoamides are both the structural moiety of biologically active compounds and important synthetic intermediates. Structurally diverse N-(2,2-diphenylvinyl)-β-oxoamides are prepared efficiently from 2-diazo-1,3-dicarbonyl compounds and N-alkyl-2,2-diphenylaziridines via an electrophilic ring opening...

An efficient synthesis of 5-halo-6-trifluoromethylpyridine-3-carbonitriles and carboxylic acids

2017 ◽  
Vol 23 (6) ◽  
Author(s):  
Manjunath B. Channapur ◽  
Roger G. Hall ◽  
Mukul Lal ◽  
Sitaram Pal ◽  
Ashok S. Shyadligeri
Keyword(s):  
Carboxylic Acids ◽  
Biologically Active Compounds ◽  
Starting Material ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Efficient Synthesis ◽  
Active Compounds

AbstractTrifluoromethyl containing heterocycles are an integral part of many biologically active compounds in the agro and pharmaceutical chemistry. Herein, we report an efficient and concise three-step synthesis of 5-halo-6-trifluoromethylpyridine-3-carbonitriles from a trifluoroacetyl vinylogous enamine starting material. Hydrolysis furnishes the carboxylic acids.

Synthesis of N-substituted Five and Six-membered Iminocyclitols-bearing Sugar Moiety: Strategy Toward the Synthesis of Pseudodisaccharide

2018 ◽  
Vol 15 (6) ◽  
pp. 853-862
Author(s):  
Nader Al Bujuq ◽  
Manuel Angulo
Keyword(s):  
Molecular Modeling ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Active Compounds ◽  
Sugar Moiety ◽  
Stereoselective Method ◽  
Glycosyl Donor ◽  
Derivatives Of ◽  
Glycosyl Donors

Aim and Objective: The efficient synthesis of disaccharide containing iminosugar moiety has a considerable interest in the field of glycoscience. In the present work, we describe a novel and applicable method for synthesis of five and six-membered N-substituted iminosugars attached with sugar moiety (pseudodisaccharides). Materials and Methods: The method of the glycosylation was based on the coupling of iminosugar thioglycoside (glycosyl donors) with partially protected sugars (glycosyl acceptors) in the presence of DMTST as a promoter. 2D COSY, HMQC, HMBC experiments were carried out to assist in NMR signal assignments. The pseudoanomeric configuration was established through NOE experiments and molecular modeling calculations. Results: Two classes of pseudodisaccharides were successfully obtained, five and six-membered N-substituted iminosugars glycosides. The six-membered pseudodisaccharides compounds were produced selectively with only β anomer. The corresponding five-membered pseudodisaccharides were achieved with moderate stereoselectivity. The yields obtained were good. These derivatives of iminocyclitols are thought to be precedents to develop various pseudodisaccharides, novel biologically active compounds, and new functional molecules. Conclusion: According to the results, utilizing iminosugar thioglycosides (1 and 2) as a glycosyl donor in glycosylation reactions is an efficient and highly stereoselective method to prepare (five- and six-membered) iminocyclitols (iminosugars) that bear a sugar moiety. The results will add to the synthesis of the iminosugars derivatives and contribute to make our approach among the few methods able to synthesize iminosugar glycosides.

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